日期:
2020 年 — 2026 年
2020
2021
2022
2023
2024
2025
2026
影响因子:

Reducing hERG Inhibition in the Design of Potent and Bioavailable Indazole cGAS Inhibitors

在设计高效且生物利用度高的吲唑类cGAS抑制剂时降低hERG抑制

Cyr, Patrick; Chefson, Amandine; Sietsema, Daniel V; Konteatis, Zenon; Ciblat, Stéphane; Sgarioto, Nicolas; Le Gros, Philippe; Pike, Kelly A; Boily, Marc-Olivier; Diallo, Mohamed; Seliniotakis, Ria; Springer, Clayton; Khandelwal, Pradhyum; Beveridge, Ramsay E

Post-symptomatic NLRP3 inhibition rescues cognitive impairment and mitigates amyloid and tau driven neurodegeneration

症状出现后抑制 NLRP3 可改善认知障碍并减轻淀粉样蛋白和 tau 蛋白驱动的神经退行性变。

Auger, Anick; Faidi, Rania; Rickman, Alexis D; Martinez, Carolina Pena; Fajfer, Austin; Carling, Jeremy; Hilyard, Addison; Ali, Mubashshir; Ono, Ryosuke; Cleveland, Connor; Seliniotakis, Ria; Truong, Nhi; Chefson, Amandine; Raymond, Marianne; Germain, Marie-Anne; Crackower, Michael A; Heckmann, Bradlee L

Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500)

发现强效且选择性的 ATR 抑制剂 Camonsertib (RP-3500)

W Cameron Black, Abbas Abdoli, Xiuli An, Anick Auger, Patrick Beaulieu, Michel Bernatchez, Cathy Caron, Amandine Chefson, Sheldon Crane, Mohamed Diallo, Stéphane Dorich, Lee D Fader, Gino B Ferraro, Sara Fournier, Qi Gao, Yelena Ginzburg, Martine Hamel, Yongshuai Han, Paul Jones, Stéphanie Lanoix, C

Identification of RP-6685, an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Polθ

鉴定出一种口服生物利用度高的化合物RP-6685,该化合物可抑制Polθ的DNA聚合酶活性。

Monica Bubenik ,Pavel Mader ,Philippe Mochirian ,Fréderic Vallée ,Jillian Clark ,Jean-François Truchon ,Alexander L Perryman ,Victor Pau ,Igor Kurinov ,Karl E Zahn ,Marie-Eve Leclaire ,Robert Papp ,Marie-Claude Mathieu ,Martine Hamel ,Nicole M Duffy ,Claude Godbout ,Matias Casas-Selves ,Jean-Pierre Falgueyret ,Prasamit S Baruah ,Olivier Nicolas ,Rino Stocco ,Hugo Poirier ,Giovanni Martino ,Alexanne Bonneau Fortin ,Anne Roulston ,Amandine Chefson ,Stéphane Dorich ,Miguel St-Onge ,Purvish Patel ,Charles Pellerin ,Stéphane Ciblat ,Thomas Pinter ,Francis Barabé ,Majida El Bakkouri ,Paranjay Parikh ,Christian Gervais ,Agnel Sfeir ,Yael Mamane ,Stephen J Morris ,W Cameron Black ,Frank Sicheri ,Michel Gallant

RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors

RP-3500:一种新型、强效且选择性的 ATR 抑制剂,在临床前模型中作为单一疗法和与 PARP 抑制剂联合使用均有效

Anne Roulston, Michal Zimmermann, Robert Papp, Alexander Skeldon, Charles Pellerin, Émilie Dumas-Bérube, Valerie Dumais, Stéphane Dorich, Lee D Fader, Sara Fournier, Li Li, Marie-Eve Leclaire, Shou Yun Yin, Amandine Chefson, Hunain Alam, William Yang, Chloe Fugère-Desjardins, Sabrina Vignini-Hammond